Treatment using dantrolene
    8.
    发明授权
    Treatment using dantrolene 有权
    使用丹曲林治疗

    公开(公告)号:US08685460B2

    公开(公告)日:2014-04-01

    申请号:US13353478

    申请日:2012-01-19

    摘要: Provided are low-volume, safe for injection formulations of dantrolene yielding significant advantages over the currently approved and marketed dantrolene for malignant hyperthermia (MH) threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. The low volume, safe for injection formulations of dantrolene have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.

    摘要翻译: 提供的低容量,安非他酮注射剂配方,与目前批准和销售的用于恶性高热(MH)威胁性麻醉危机的丹曲林相比,具有显着的优势。 一旦丹培罗林可以立即提供给触发MH的患者立即使用,麻醉师将能够专注于在这个复杂而不断演变的危机中对患者生理状况的管理,而不是在救援人员的费力和耗时的重组过程中。 丹那罗林注射剂配方的体积小,安全性高于目前使用的泵头预防和治疗方法,以及其他神经系统,认知功能障碍和运动功能障碍对医源性或创伤引起的血流变化情况的影响,包括外科手术 涉及CPB或相关程序的程序,以及在非正常体温发作期间由医源性或疾病引起的程序。

    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1
    10.
    发明申请
    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 失效
    制备1型11β-羟基类固醇脱氢酶的C-5-取代的杂环抑制剂的催化方法

    公开(公告)号:US20070117985A1

    公开(公告)日:2007-05-24

    申请号:US11590922

    申请日:2006-11-01

    CPC分类号: C07D277/54 C07D277/42

    摘要: The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

    摘要翻译: 本发明提供了在碱存在下通过式1化合物与式R 2 LG化合物之间的催化反应来制备式II的11β-羟基类固醇脱氢酶1型抑制剂的方法: 其中R 1,R 2,X,Y和LG在说明书中描述。 示例性催化剂含有钯和一种或多种膦配体。 该方法可以以立体选择性方式进行,得到对映异构体富集的产物。